Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor
Wang, Xiaolun, Allen, Shelley, Blake, James F, Bowcut, Vickie, Briere, David M, Calinisan, Andrew, Dahlke, Joshua R, Fell, Jay B, Fischer, John P, Gunn, Robin J, Hallin, Jill, Laguer, Jade, Lawson, J. David, Medwid, James, Newhouse, Brad, Nguyen, Phong, O’Leary, Jacob M, Olson, Peter, Pajk, Spencer, Rahbaek, Lisa, Rodriguez, Mareli, Smith, Christopher R, Tang, Tony P, Thomas, Nicole C, Vanderpool, Darin, Vigers, Guy P, Christensen, James G, Marx, Matthew A
Published in Journal of medicinal chemistry (24.02.2022)
Published in Journal of medicinal chemistry (24.02.2022)
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MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody
Farrell, Pamela J, Matuszkiewicz, Jennifer, Balakrishna, Deepika, Pandya, Shweta, Hixon, Mark S, Kamran, Ruhi, Chu, Shaosong, Lawson, J David, Okada, Kengo, Hori, Akira, Mizutani, Akio, Iwata, Hidehisa, de Jong, Ron, Hibner, Barbara, Vincent, Patrick
Published in Molecular cancer therapeutics (01.07.2017)
Published in Molecular cancer therapeutics (01.07.2017)
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Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design—Part 2
McBride, Christopher, Cheruvallath, Zacharia, Komandla, Mallareddy, Tang, Mingnam, Farrell, Pamela, Lawson, J. David, Vanderpool, Darin, Wu, Yiqin, Dougan, Douglas R., Plonowski, Artur, Holub, Corine, Larson, Chris
Published in Bioorganic & medicinal chemistry letters (15.06.2016)
Published in Bioorganic & medicinal chemistry letters (15.06.2016)
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Protein flexibility and intrinsic disorder
Radivojac, Predrag, Obradovic, Zoran, Smith, David K., Zhu, Guang, Vucetic, Slobodan, Brown, Celeste J., Lawson, J. David, Dunker, A. Keith
Published in Protein science (01.01.2004)
Published in Protein science (01.01.2004)
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DisProt: a database of protein disorder
Vucetic, Slobodan, Obradovic, Zoran, Vacic, Vladimir, Radivojac, Predrag, Peng, Kang, Iakoucheva, Lilia M., Cortese, Marc S., Lawson, J. David, Brown, Celeste J., Sikes, Jason G., Newton, Crystal D., Dunker, A. Keith
Published in Bioinformatics (01.01.2005)
Published in Bioinformatics (01.01.2005)
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Molecular dynamics analysis of structural factors influencing back door pi release in myosin
Lawson, J David, Pate, Edward, Rayment, Ivan, Yount, Ralph G
Published in Biophysical journal (01.06.2004)
Published in Biophysical journal (01.06.2004)
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Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers
Smith, Christopher R, Aranda, Ruth, Bobinski, Thomas P, Briere, David M, Burns, Aaron C, Christensen, James G, Clarine, Jeffery, Engstrom, Lars D, Gunn, Robin J, Ivetac, Anthony, Jean-Baptiste, Ronald, Ketcham, John M, Kobayashi, Masakazu, Kuehler, Jon, Kulyk, Svitlana, Lawson, J. David, Moya, Krystal, Olson, Peter, Rahbaek, Lisa, Thomas, Nicole C, Wang, Xiaolun, Waters, Laura M, Marx, Matthew A
Published in Journal of medicinal chemistry (10.02.2022)
Published in Journal of medicinal chemistry (10.02.2022)
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Journal Article
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein–Protein Interaction
Ketcham, John M., Haling, Jacob, Khare, Shilpi, Bowcut, Vickie, Briere, David M., Burns, Aaron C., Gunn, Robin J., Ivetac, Anthony, Kuehler, Jon, Kulyk, Svitlana, Laguer, Jade, Lawson, J. David, Moya, Krystal, Nguyen, Natalie, Rahbaek, Lisa, Saechao, Barbara, Smith, Christopher R., Sudhakar, Niranjan, Thomas, Nicole C., Vegar, Laura, Vanderpool, Darin, Wang, Xiaolun, Yan, Larry, Olson, Peter, Christensen, James G., Marx, Matthew A.
Published in Journal of medicinal chemistry (28.07.2022)
Published in Journal of medicinal chemistry (28.07.2022)
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Journal Article
Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton’s Tyrosine Kinase
Smith, Christopher R., Dougan, Douglas R., Komandla, Mallareddy, Kanouni, Toufike, Knight, Beverly, Lawson, J. David, Sabat, Mark, Taylor, Ewan R., Vu, Phong, Wyrick, Corey
Published in Journal of medicinal chemistry (23.07.2015)
Published in Journal of medicinal chemistry (23.07.2015)
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Journal Article
Exploration of Cryptic Pockets Using Enhanced Sampling Along Normal Modes: A Case Study of KRAS G12D
Vithani, Neha, Zhang, She, Thompson, Jeffrey P, Patel, Lara A, Demidov, Alex, Xia, Junchao, Balaeff, Alexander, Mentes, Ahmet, Arnautova, Yelena A, Kohlmann, Anna, Lawson, J David, Nicholls, Anthony, Skillman, A Geoffrey, LeBard, David N
Published in Journal of chemical information and modeling (17.10.2024)
Published in Journal of chemical information and modeling (17.10.2024)
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Journal Article
Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)‑5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro‑3H‑1,2,4-triazol-3-one, by Fragment-Based Drug Design
Sabat, Mark, Dougan, Douglas R, Knight, Beverly, Lawson, J. David, Scorah, Nicholas, Smith, Christopher R, Taylor, Ewan R, Vu, Phong, Wyrick, Corey, Wang, Haixia, Balakrishna, Deepika, Hixon, Mark, Madakamutil, Loui, McConn, Donavon
Published in Journal of medicinal chemistry (09.09.2021)
Published in Journal of medicinal chemistry (09.09.2021)
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Journal Article
Correction to “Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)‑5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro‑3H‑1,2,4-triazol-3-one, by Fragment-Based Drug Design”
Sabat, Mark, Dougan, Douglas R, Ermolieff, Jacques, Halkowycz, Petro, Knight, Beverly, Lawson, J. David, Scorah, Nicholas, Smith, Christopher R, Taylor, Ewan R, Vu, Phong, Wyrick, Corey, Wang, Haixia, Balakrishna, Deepika, Hixon, Mark, Madakamutil, Loui, McConn, Donavon
Published in Journal of medicinal chemistry (11.11.2021)
Published in Journal of medicinal chemistry (11.11.2021)
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Journal Article
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X‑Ray Cocrystallography
Smith, Christopher R., Chen, Dan, Christensen, James G., Coulombe, René, Féthière, James, Gunn, Robin J., Hollander, Johan, Jones, Benjamin, Ketcham, John M., Khare, Shilpi, Kuehler, Jon, Lawson, J. David, Marx, Matthew A., Olson, Peter, Pearson, Kelly E., Ren, Cynthia, Tsagris, Denise, Ulaganathan, Thirumalaiselvi, Van’t Veer, Inge, Wang, Xiaolun, Ivetac, Anthony
Published in Journal of medicinal chemistry (11.01.2024)
Published in Journal of medicinal chemistry (11.01.2024)
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Journal Article
Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitors
Smith, Christopher R., Aranda, Ruth, Christensen, James G., Engstrom, Lars D., Gunn, Robin J., Ivetac, Anthony, Ketcham, John M., Kuehler, Jon, David Lawson, J., Marx, Matthew A., Olson, Peter, Thomas, Nicole C., Wang, Xiaolun, Waters, Laura M., Kulyk, Svitlana
Published in Bioorganic & medicinal chemistry (01.10.2022)
Published in Bioorganic & medicinal chemistry (01.10.2022)
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Journal Article
The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading
Sudhakar, Niranjan, Yan, Larry, Qiryaqos, Fadia, Engstrom, Lars D, Laguer, Jade, Calinisan, Andrew, Hebbert, Allan, Waters, Laura, Moya, Krystal, Bowcut, Vickie, Vegar, Laura, Ketcham, John M, Ivetac, Anthony, Smith, Christopher R, Lawson, J David, Rahbaek, Lisa, Clarine, Jeffrey, Nguyen, Natalie, Saechao, Barbara, Parker, Cody, Elliott, Adam J, Vanderpool, Darin, He, Leo, Hover, Laura D, Fernandez-Banet, Julio, Coma, Silvia, Pachter, Jonathan A, Hallin, Jill, Marx, Matthew A, Briere, David M, Christensen, James G, Olson, Peter, Haling, Jacob, Khare, Shilpi
Published in Molecular cancer therapeutics (01.10.2024)
Published in Molecular cancer therapeutics (01.10.2024)
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Identification of AHCY inhibitors using novel high-throughput mass spectrometry
Uchiyama, Noriko, Dougan, Douglas R., Lawson, J. David, Kimura, Hitomi, Matsumoto, Shin-ichi, Tanaka, Yukiya, Kawamoto, Tomohiro
Published in Biochemical and biophysical research communications (09.09.2017)
Published in Biochemical and biophysical research communications (09.09.2017)
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Journal Article
The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading
Sudhakar, Niranjan, Yan, Larry, Qiryaqos, Fadia, Engstrom, Lars D, Laguer, Jade, Calinisan, Andrew, Hebbert, Allan, Waters, Laura, Moya, Krystal, Bowcut, Vickie, Vegar, Laura, Ketcham, John M, Ivetac, Anthony, Smith, Christopher R, Lawson, J David, Rahbaek, Lisa, Clarine, Jeffrey, Nguyen, Natalie, Saechao, Barbara, Parker, Cody, Elliott, Adam J, Vanderpool, Darin, He, Leo, Hover, Laura D, Fernandez-Banet, Julio, Coma, Silvia, Pachter, Jonathan A, Hallin, Jill, Marx, Matthew A, Briere, David M, Christensen, James G, Olson, Peter, Haling, Jacob, Khare, Shilpi
Published in Molecular cancer therapeutics (21.06.2024)
Published in Molecular cancer therapeutics (21.06.2024)
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Journal Article
MRTX1719 Is an MTA-Cooperative PRMT5 Inhibitor That Exhibits Synthetic Lethality in Preclinical Models and Patients with MTAP-Deleted Cancer
Engstrom, Lars D, Aranda, Ruth, Waters, Laura, Moya, Krystal, Bowcut, Vickie, Vegar, Laura, Trinh, David, Hebbert, Allan, Smith, Christopher R, Kulyk, Svitlana, Lawson, J David, He, Leo, Hover, Laura D, Fernandez-Banet, Julio, Hallin, Jill, Vanderpool, Darin, Briere, David M, Blaj, Alice, Marx, Matthew A, Rodon, Jordi, Offin, Michael, Arbour, Kathryn C, Johnson, Melissa L, Kwiatkowski, David J, Jänne, Pasi A, Haddox, Candace L, Papadopoulos, Kyriakos P, Henry, Jason T, Leventakos, Konstantinos, Christensen, James G, Shazer, Ronald, Olson, Peter
Published in Cancer discovery (01.11.2023)
Published in Cancer discovery (01.11.2023)
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Journal Article
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein
Ketcham, John M., Harwood, Stephen J., Aranda, Ruth, Aloiau, Athenea N., Bobek, Briana M., Briere, David M., Burns, Aaron C., Caddell Haatveit, Kersti, Calinisan, Andrew, Clarine, Jeffery, Elliott, Adam, Engstrom, Lars D., Gunn, Robin J., Ivetac, Anthony, Jones, Benjamin, Kuehler, Jon, Lawson, J. David, Nguyen, Natalie, Parker, Cody, Pearson, Kelly E., Rahbaek, Lisa, Saechao, Barbara, Wang, Xiaolun, Waters, Anna, Waters, Laura, Watkins, Ashlee H., Olson, Peter, Smith, Christopher R., Christensen, James G., Marx, Matthew A.
Published in Journal of medicinal chemistry (28.03.2024)
Published in Journal of medicinal chemistry (28.03.2024)
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